Design, Synthesis, and Preclinical Characterization of the Selective Androgen Receptor Modulator (SARM) RAD140

  • ACS Med Chem Lett. 2010 Dec 2;2(2):124-9. doi: 10.1021/ml1002508.
Chris P Miller  1 ,  Maysoun Shomali  1 ,  C Richard Lyttle  1 ,  Louis St L O'Dea  1 ,  Hillary Herendeen  1 ,  Kyla Gallacher  1 ,  Dottie Paquin  1 ,  Dennis R Compton  2 ,  Bishwabhusan Sahoo  2 ,  Sean A Kerrigan  2 ,  Matthew S Burge  2 ,  Michael Nickels  2 ,  Jennifer L Green  2 ,  John A Katzenellenbogen  3 ,  Alexei Tchesnokov  4 ,  Gary Hattersley  1
Affiliations
  • 1. Radius Health, Inc., 300 Technology Square, Cambridge, Massachusetts 02139, United States.
  • 2. Obiter Research, 2809 Gemini Court, Champaign, Illinois 61822-9647, United States.
  • 3. Department of Chemistry, University of Illinois at Urbana-Champaign, 600 South Mathews Avenue, Urbana, Illinois 61801, United States.
  • 4. Cambridge Major Laboratories, Inc., W130 N10497 Washington Drive, Germantown, Wisconsin 53022, United States.
PMID: 24900290 DOI: 10.1021/ml1002508
Abstract

This report describes the discovery of RAD140, a potent, orally bioavailable, nonsteroidal selective Androgen Receptor Modulator (SARM). The characterization of RAD140 in several preclinical models of anabolic androgen action is also described.

Keywords
Androgen; Herschberger assay; SARM; cachexia; oxadiazole; primate.
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